Title : The effect of breast cancer resistance protein, multidrug resistant protein 1, and organic anion-transporting polypeptide 1B3 on the antitumor efficacy of the lipophilic camptothecin 7-t-butyldimethylsilyl-10-hydroxycamptothecin (AR-67) in vitro.

Pub. Date : 2013 Jul

PMID : 23620484






3 Functional Relationships(s)
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1 Using cell lines expressing the aforementioned transporters, we showed that the lipophilic AR-67 lactone form is a substrate for efflux transporters BCRP and MDR1. Lactones ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus
2 Notably, both BCRP and MDR1 conferred resistance to AR-67 lactone. Lactones ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus
3 In conclusion, BCRP- and MDR1-mediated efflux of AR-67 lactone confers resistance to AR-67, but OATP1B3-mediated uptake of the AR-67 carboxylate does not sensitize OATP1B3-expressing tumor cells. Lactones ATP binding cassette subfamily G member 2 (Junior blood group) Mus musculus